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Glycyrrhetinic acid derivative and vardenafil compound chewable tablet

A technology of glycyrrhetinic acid and vardenafil, which is applied in the direction of drug combinations, pharmaceutical formulas, active ingredients of heterocyclic compounds, etc., can solve the problem that the anti-tumor activity of the compound is not obvious, so as to improve the anti-ED effect, improve the therapeutic effect, The effect of increasing selectivity

Inactive Publication Date: 2018-01-19
陈有平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Vardenafil (Vardenafil) is a selective PDE5 inhibitor developed by Bayer (Bayer) and Glaxo Smith Kline (Glaxo Smith Kline). The characteristics of fast effective time and high safety, Chinese patent CN201110131028.5 discloses 2-cyano-3-oxo-18β-oleanane-1,12-diene- 30-methyl carboxylate (I), and it has certain antitumor activity, but in this document, the antitumor activity of this compound is not obvious

Method used

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  • Glycyrrhetinic acid derivative and vardenafil compound chewable tablet
  • Glycyrrhetinic acid derivative and vardenafil compound chewable tablet
  • Glycyrrhetinic acid derivative and vardenafil compound chewable tablet

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1～4

[0015] Preparation examples 1-4, compound chewable tablets of vardenafil and 2-methoxy-3-oxo-18β-oleanane-1,12-diene-30-acid (referred to as compound (I))

[0016]

[0017] The chemical formula of compound (I) is as follows

[0018]

[0019] The synthesis method of compound (I) is as described in CN201110131028.5.

[0020] The preparation method of the chewable tablet in the preparation example is as follows:

[0021] (1) Accurately weigh part of the raw and auxiliary materials (principal drug, binder, filler and disintegrating agent) according to the prescription ratio, pass through a 100-mesh sieve, mix thoroughly, add 50% ethanol in an appropriate amount to prepare a soft material, and use 24 Granulate with a mesh sieve, dry at 60°C, and granulate with a 24-mesh sieve.

[0022] (2) Add flavoring agent and lubricant to the above-mentioned sized granules, mix well, adjust tablet weight, and compress.

Embodiment 1

[0023] Pharmacological embodiment 1PDEs selectivity test

[0024] PDE6 is extracted from bovine retina, PDE3 and PDE5 are extracted from rabbit platelets, PDE4 is extracted from male SD rat kidney, PDE1 is extracted from male SD rat brain cortex, and PDE2 is extracted from beagle dog adrenal gland

[0025] PDEs activity test method

[0026] Vardenafil and compound (I) were prepared with DMSO concentration as a stock solution of 100mM, and then diluted with purified water in the ratio shown in the table below Mixed solution, the concentration of the mixed solution of experimental groups 1 to 7 was 10mM, 1mM, 100μM, 10μM, 1μM, 100nM, 10nM, 1nM, 0.1nM in terms of vardenafil, and the solutions of experimental groups 8 and 9 were respectively vardenafil Nafil and compound (I) stock solutions were diluted with purified water to solutions with concentrations of 10 mM, 1 mM, 100 μM, 10 μM, 1 μM, 100 nM, 10 nM, 1 nM, and 0.1 nM.

[0027]

[0028] According to different enzymes, ch...

Embodiment 2

[0037] Pharmacological Example 2 In Vivo Drug Efficacy Experiment

[0038] 2.1. Animal grouping

[0039] Male mature rabbits with a body weight of 3.5-4.5 kg were randomly divided into groups of 10. The grouping and administration conditions are shown in the table below:

[0040] Group No

Drug administration

1

(Blank control) Physiological saline 4ml / kg

2

(Positive control) Vardenafil 10mg / kg

3

Vardenafil 5mg / kg+ Compound (I) 5mg / kg

4

Vardenafil 5mgkg+ Compound (I) 7.5mg / kg

5

Vardenafil 5mg / kg+ Compound (I) 10mg / kg

6

Vardenafil 5mg / kg+ Compound (I) 12mg / kg

[0041] 2.3 Test method

[0042] SNP (sodium nitroprusside) as an exogenous NO donor was injected into the marginal ear vein, the administration volume was 1 ml / kg, and the SNP concentration of the injection was 0.1 μmol / L.

[0043] After weighing the rabbits, carry out intragastric administration according to the dosage plan in 2.1 above with a ...

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Abstract

The invention relates to a glycyrrhetinic acid derivative and vardenafil compound chewable tablet, which is characterized in that the chewable tablet is prepared from active ingredients and medical auxiliary materials applicable to the chewable tablet. The active ingredients are prepared from vardenafil and 2-cyano-3-oxo-18beta-oleanane-1,12-diene-30-methyl carbonate according to the mass ratio of1:(1.5 to 2); the medical auxiliary materials are prepared from 3 to 4 percent of disintegrants, 3 to 5 percent of bonding agents, 0.5 to 3 percent of flavoring agents, 0.5 to 1 percent of lubricating agents and the balance of filling agents (accounting for the total mass of the medical auxiliary materials).

Description

Technical field: [0001] The invention relates to a compound oral preparation of vardenafil and glycyrrhetinic acid derivatives. Background technique: [0002] Vardenafil (Vardenafil) is a selective PDE5 inhibitor developed by Bayer (Bayer) and Glaxo Smith Kline (Glaxo Smith Kline). The characteristics of fast effective time and high safety, Chinese patent CN201110131028.5 discloses 2-cyano-3-oxo-18β-oleanane-1,12-diene- 30-methyl carboxylate (I), and it has certain antitumor activity, but in this document, the antitumor activity of this compound is not obvious. The chemical formula of the compound (I) is [0003] [0004] In the previous experiments, we found that compound (I) can increase the selective inhibition of vardenafil on PDE5, so on this basis, it has become a reality to provide a compound preparation of glycyrrhetinic acid derivatives and vardenafil with a suitable ratio. There are problems that need to be solved in technology. Contents of the invention ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K31/53A61K9/20A61K47/38A61K47/36A61P15/10
Inventor 陈有平
Owner 陈有平
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